TDI-11861

TDI-11861 : Inhibitor of ADCY10

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe TDI-11861 is in the process of SERP review.

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Information

ADCY10

Inhibitor

up to 100 nM

In Vitro Validations

Uniprot ID: Q96PN6

Target Class: Enzyme

Target SubClass: Cyclase

Potency: Kd

Potency Value: 1.4 nM

Potency Assay: SPR; also increased residence time of 3181 s

PDB ID for probe-target interaction (3D structure): 8B75

Target aliases:

Adenylate cyclase type 10, SAC, ADCY10, ADCYA_HUMA ...

DOI Reference: 10.1021/acs.jmedchem.2c01133

Uniprot ID: Q96PN6

Target Class: Enzyme

Target SubClass: Cyclase

Potency: IC50

Potency Value: 3.3 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): 8B75

Target aliases:

Adenylate cyclase type 10, SAC, ADCY10, ADCYA_HUMA ...

DOI Reference: 10.1021/acs.jmedchem.2c01133

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): TDI-11861 retained high selectivity for sAC vs closely related tmAC family members. TDI-11861 did not show appreciable activity against a panel of 322 kinases and 46 other relevant drug targets such as GPCRs, ion channels, and nuclear receptors in a Eurofins safety panel.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The compound has a short half-life and low bioavailability.

(last updated: 2 Apr 2025 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

For longer term dosing (42 days), the authors utilized TDI-11155, which provided improved solubility relative to TDI-11861 to allow for use in an osmotic pump. While the IV clearance of the compound is high in mouse, the current probe can be utilized either via IP or oral gavage at 50 mpk to observe the desired in vivo efficacy in male mice. The compound is potent in both biochemical and cell assays with a long residence time and shows a high level of selectivity for this target.

(last updated: 23 Jun 2025 )